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Synthesis and Biological Activity of 28-Amide Derivatives of 23-Hydroxy Betulinic Acid as Antitumor Agent Candidates

[ Vol. 9 , Issue. 7 ]


Yi Bi, Jinyi Xu, Fei Sun, Xiaoming Wu, Wencai Ye, Yijun Sun and Wenwen Huang   Pages 920 - 925 ( 6 )


Based on the structure of 23-hydroxybetulinic acid (1), a series of 28-amide derivatives were synthesized. Biological evaluation in vitro for their antitumor activities against five cell lines (A549, BEL-7402, SF-763, B16 and HL-60) has indicated that compound 6g possesses the most effective antitumor activity with an IC50 value of 10.47 μM when treated with HL-60 cells. In vivo testing has also shown a comparable activity of 6g to cyclophosphamide against H22 liver tumor in mice and 5-fluorouracil against B16 melanoma, respectively.


23-hydroxy betulinic acid, 28-carboxylic acid, amide derivatives, antitumor activity.


Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, 210009 Jiangsu, China and Center for Drug Discovery, College of Pharmacy, China Pharmaceuticcl University, Nanjing, 210009 Jiangsu, China.

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